Drug intelligence / Profile preview

trastuzumab rezetecan + retlirafusp alfa

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

SHR-A1811 (trastuzumab rezetecan) is a third-generation HER2-targeted antibody-drug conjugate (ADC) that delivers a cytotoxic payload to HER2-expressing tumor cells. Its mechanism of action involves targeting the human epidermal growth factor receptor 2 (HER2) and delivering a DNA topoisomerase I inhibitor to induce cell death in cancer cells. It has demonstrated efficacy in HER2-mutant non-small cell lung cancer and HER2-positive breast cancer, among other solid tumors[1][5][8]. SHR-1701 (retlirafusp alfa) is a bifunctional fusion protein that targets both programmed death-ligand 1 (PD-L1) and transforming growth factor beta (TGF-β), thereby blocking immune checkpoint signaling and modulating the tumor microenvironment to enhance antitumor immunity[3][4]. The combination of these two agents represents an investigational regimen for advanced or metastatic solid tumors, leveraging both targeted cytotoxicity and immunomodulation.

Other names
trastuzumab rezetecanretlirafusp alfa
02

Targets

TGFB (GARP–latent transforming growth factor beta 1 complex)ERBB2 (Erb-b2 receptor tyrosine kinase 2)CD274 (Programmed cell death protein 1 ligand 1)TOP1 (DNA Topoisomerase I)

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